A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.
Bioorg Med Chem Lett
; 22(8): 2811-7, 2012 Apr 15.
Article
en En
| MEDLINE
| ID: mdl-22444683
ABSTRACT
A new structural class of potent prolylcarboxypeptidase (PrCP) inhibitors was discovered by high-throughput screening. The series possesses a tractable SAR profile with sub-nanomolar in vitro IC(50) values. Compared to prior inhibitors, the new series demonstrated minimal activity shifts in pure plasma and complete ex vivo plasma target engagement in mouse plasma at the 20 h post-dose time point (po). In addition, the in vivo level of CNS and non-CNS drug exposure was measured.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Carboxipeptidasas
/
Inhibidores Enzimáticos
/
Descubrimiento de Drogas
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Estados Unidos